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What are opiates?
Pharmacologically active compounds derived naturally from opium
What is the scientific name of the opium plant?
Papaver somniferum
Where was opium first cultivated?
Mediterranean region
Which country has a major involvement in the licit production of opiates?
India
Name five alkaloids found in the opium plant.
Morphine, codeine, noscapine, papaverine, thebaine
List three major factors that popularized opiate abuse in the US.
The unrestricted availability of opium.
The influx of opium-smoking immigrants from Asia.
Invention of the hypodermic needle which facilitated a more severe variety of compulsive drug abuse
Morphine is produced in the opium plant as the enantiomerically pure _ isomer.
levorotatory
What is the most commonly abused opiate in the US?
Heroin
What is the primary source of heroin in the US?
Clandestine synthesis involving acetylation of morphine
Which opiate, derived from a nuclear modification of morphine, is 1000 times as potent as morphine?
Oripavines including etorphine
T/F Dextromethorphan is a non-addicting antitussive agent, but it is a Schedule III controlled substance.
False
What is buprenorphine?
Potent partial opiate agonist indicated for the relief of moderate to severe pain in humans
For what use was meperidie (pethidine) originally synthesized?
As a potential antispasmodic
Define agonist; name one.
is a term used to describe a type of drug that binds and alters the activity of a receptor
Pentazocine
Describe what an antagonist is and what it does; name one.
A receptor antagonist is a type of receptor drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses
Naloxone and naltrexone
How does the analgesic property of opiates work?
Analgesics, by definition, are medicinal agents that alter an individual’s reaction to painful stimuli by interfering with the neural or chemical transmission of the stimuli. The analgesic effects of the opiates are usually accompanied by a narcotic action characterized by drowsiness, sedation, changes in mood and mental clouding
Name two opiates that are bicyclic derivatives of morphine.
Meperidine (pethididne)
Alaphaprodine
Fentanyl
⍺-methylfentanyl
Methadone
propoxyphene
Define antitussive
Management of the cough syndrome by opiates
What is the most common affective (emotional) response to the opiates?
Euphoria
When someone overdoses on opiates, death is usually caused by what?
Respiratory failure
T/F One effect of opiate use is miosis.
True
Define miosis.
Constriction of the pupils
What causes psychological dependance on opiates?
The euphoria associated with opiate use induces a powerful compulsion to continue use of the drug
Name three effects of opiates that develop at a high degree of tolerance?
Mental clouding
Sedation
Nausea and vomiting
T/F Miosis develops a moderate degree of tolerance after prolonged use of opiates.
False, miosis is seen in minimal or no tolerance
What causes withdrawal symptoms?
Due to a failure to continue administration of an opiate to which an individual has developed physical dependence
What is tolerance?
Upon frequent administration there is a gradual loss in intensity of several of the pharmacological effects of the opiates. This phenomenon is termed tolerance
List what schedule the following drugs are in:
Hydrocodone: Schedule 2
Dihydrocodeinone: Schedule 3
Oxycodone: Schedule 2
Oxycodone with acetaminophen: Schedule 2
Alpha-methylfentanyl: Schedule 1
Fentanyl: Schedule 2
Buprenorphine: Schedule 3
Dextromethorphan: NC
Naloxone: NC
Heroin: Schedule 1
Butorphanol: Schedule 4
Diphenoxylate: Schedule 5
Raw opium: Schedule 2
Hydromorphone: Schedule 2
Define diluent.
Compounds added strictly for “bulk” to increase the quantity of powder for distribution.
Define adultrant.
Compounds added to either increase the effect of the heroin on the body or to fool the pusher and/or addict into thinking they have a better quality product.
How is the separation of hydrocodone from acetaminophen accomplished?
Separation of hydrocodone from acetaminophen is accomplished by grinding the tablet or removing the contents of a capsule preparation and placing in a filter paper cone and washing with freshly prepared n--hexane that has been saturated with ammonium hydroxide. The hexane solution is evaporated to dryness and the residue that remains is hydrocodone.
Which isomer of propoxyphene is controlled?
Dextropropoxyphene
What is the best method of analysis for opiates?
GC/MS